Recent advances in basic biomedical research have clarified our understanding of human disease states and provided tools for the derivation of effective therapies. For example, specific inhibitors can be designed to fit three-dimensional crystal structures; phage libraries can be screened for ligand-binding activity; and gene functions associated with transformation can be manipulated for the discovery of antineoplastic compounds. Given an expanding array of potentially useful therapeutic compounds, it becomes ever more critical that time-efficient and accurate processes are in place to guide selection of those entities that will be taken into the clinic. In addition, an increasing diversity of therapeutic applications will pose novel challenges for regulatory agencies, for the implementatation and interpretation of clinical trials, and for the cost-effective introduction of new therapeutic products in the market. The intent of the proposed meeting is to counterpoint the power of the current scientific discovery process with the limitations of existing paradigms of drug development. Planned sessions will address a spectrum of issues, ranging from methods for preclinical drug evaluation in vitro and in vivo, to pharmacologic considerations necessary for preclinical and early clinical tests, to systems which might facilitate the planning, implementation, and interpretation of clinical trials. In addition, regulatory perspectives and principles germane to the development process as well as economic models for cost-effective introduction and evaluation of new therapeutic compounds will be discussed. As a primary goal, leaders from the various arenas of drug development, including academic, biotechnology, major pharmaceutical companies, and the FDA, will critically evaluate current paradigms for moving novel compounds from the lab-bench to the clinic. In so doing, it is hoped that this symposium win spark innovative approaches to remove outstanding obstacles and to expedite the development of effective therapies in the future.